Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: Itraconazole

Taupitz, Thomas; Dressman, Jennifer B.; Buchanan, Charles M.; Klein, Sandra

doi:10.1016/j.ejpb.2012.11.003

Cited by 105 publications

(69 citation statements)

References 34 publications

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“…Therefore, several techniques to improve solubility of poorly water-soluble drugs have been developed: inclusion complexes in cyclodextrins (Joudieh et al, 2009), self-emulsifying drug delivery systems (Porter et al, 2008), nanocrystals (Junghanns and Muller, 2008;Shegokar and Muller, 2010), coacervation (De Jaeghere et al, 2013), solid dispersions (Janssens and Van den Mooter, 2009). The latter technique (where the drug is (molecularly) dispersed in a carrier) can be prepared via solvent evaporation (Dave et al, 2012), fusion methods (Gorajana et al, 2013), complexation (Taupitz et al, 2013), spray-drying (Jang et al, 2013) or hot-melt extrusion . For pharmaceutical applications hot-melt extrusion (HME) is considered an effective process to formulate immediate release forms of poorly water-soluble drugs via the formation of solid dispersions or solutions since it has many advantages over conventional approaches, such as a solvent-free process, the possibility to be operated as continuous process, a limited number of processing steps (Maniruzzaman et al, 2013;Repka et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

Jaeghere

Beer

Bocxlaer

et al. 2015

International Journal of Pharmaceutics

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The primary purpose of this study was to process partially hydrolyzed PVOH grades (degree of hydroxylation (DH): 33-88%) via HME and to evaluate them as carrier for oral immediate release dosage forms in order to improve the release rate of poorly water soluble drugs (i.e.HCT and CEL) via the formulation of solid dispersions. PVOH grades (DH > 70%) were able to solubilize HCT and CEL up to 15%, but required higher extrusion temperature, due to the crystalline nature of PVOH. The highest drug release rate was observed from hot-melt extruded PVOH samples with a high DH. While drug release from extrudates consisting of PVOH with a low DH was affected by ionic strength, there was no influence of pH and ionic strength on HCT release from PVOH samples with a higher DH. However, PVOH (DH > 70%) required higher extrusion temperatures, which could hamper its application for thermosensitive drugs. Therefore, the secondary purpose was to investigate the effect of sorbitol, a water-soluble plasticizer, on the thermal properties of hot-melt extruded PVOH (DH > 70%). The melting of PVOH/sorbitol mixture was required to establish molecular interactions between PVOH and sorbitol. These molecular interactions were reflected in the HME behavior: whereas an extrusion temperature of 180°C was necessary to process physical mixtures of PVOH (DH > 70%) and sorbitol, only 140°C was necessary during reextrusion (after quench cooling and cryomilling) of the PVOH/sorbitol mixture. In addition, the in vitro and in vivo dug release of plasticized PVOH was examined; whereas the CEL/PVOH/sorbitol system was able to maintain supersaturation during in vitro dissolution (0.1 N HCl) compared to Celebrex ® , the in vivo pharmacokinetic parameters (AUC 0-24h , C max and T max ) were highly comparable.

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Section: Introductionmentioning

confidence: 99%

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

Jaeghere

Beer

Bocxlaer

et al. 2015

International Journal of Pharmaceutics

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“…Recently, complexation with cyclodextrins has been reported to enhance the solubility and dissolution rate of itraconazoe (Taupitz et al, 2013), curcumin (Michel et al, 2012), repaglanide (Liu et al, 2014), and myricetin (Yao et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

PREPERATION AND CHARACTERIZATION OF Β-Cyclodextrin INCLUSION COMPLEXES ORAL TABLETS CONTAINING POORLY WATER SOLUBLE GLIMIPIRIDE USING FREEZE DRYING METHOD

Syukri

Fernenda,

Utami

et al. 2015

Indonesian J. Pharm.

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Glimepiride is an oral antidiabetic drugs which is practically insoluble in water. The formation of β-cyclodextrin inclusion complex was able to increase the solubility of glimepiride. This study aim to prepare, characterize and formulation of inclusion complex tablets in order to meet the requirement in Pharmacopeia. The inclusion complex were prepared in a molar ratio of 1:1 and 1:2 by freeze drying method, after that characterized include FTIR spectroscopy and scanning electro microscope (SEM). Further, it was formulated into tablets by direct compression technique using primogel and crospovidone as super disintegrants. The tablets were evaluated include weight uniformity, hardness, friability, disintegration, and dissolution. The dissolution studies of inclusion complex were performed by using USP II apparatus. The result of FTIR and SEM provided evidence of the formation of complexes after utilizing freeze-drying methods. The tablet evaluation containing inclusion complex glimepiride-β cyclodextrin with primogel and cropovidone as disintegrant showed that increased concentration of disintegrant will increase disintegration time of the tablets. All of formulas meet the requirements in the Pharmacopoeia. The inclusion complex of glimepiride-β cyclodextrin successfully used for enhancing the solubility of glimepiride and the tablets meet the requirement in Pharmacopeia.

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“…Addition of small amounts of water soluble polymers to the drug cyclodextrin binary systems are known to improve both the complexing and solubilizing efficiencies of cyclodextrins [19][20][21][22] . Ternary inclusion complexes of beta-cyclodextrin derivatives with sodium carboxymethyl cellulose (CMC) with have been reported for Rofecoxib 23 , Nimuselide 24 , cefpodoxime 25 , Budesonide 26 and Tropicamide 27 in order to improve their solubility or therapeutic responses.…”

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confidence: 99%

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2016

IJPSR

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ABSTRACT:The objective of the present investigation was to study the complexation of silymarin, a poorly water soluble herbal drug, with β-cyclodextrin alone and in the presence of sodium carboxymethyl cellulose to evaluate the feasibility of enhancing the solubility and dissolution rate of silymarine. Phase solubility study and kneading method was employed to develop and formulate solid inclusion complexes. Solid inclusion complexes of silymarin -β-cyclodextrin in 1:1 molar ratio were prepared with and without carboxymethyl cellulose by kneading method. Obtained binary and ternary complexes were evaluated for solubility dissolution and physical nature by FTIR, XRD and NMR. The aqueous solubility of silymarin was linearly increased as a function of the concentration of β-cyclodextrin alone and in the presence of sodium carboxymethyl cellulose. Beta cyclodextrin formed binary molecular inclusion complexes with silymarin in1:1 molar ratio as revealed by phase solubility diagram. Sodium carboxymethyl cellulose in ternary complexes has resulted in 2.37 and 1.66 fold enhancements in complexation and solubilizing efficiencies of β-cyclodextrin respectively. Dissolution rate of silymarin in binary and ternary complexes was enhanced up to 1.3 and 1.6 folds respectively when compared with pure silymarin. It is evident that addition of sodium carboxymethyl cellulose affects the complexation and solubilizing efficiencies of β-cyclodextrin hence it may be used in solid dispersions to minimize the overall formulation bulk.

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Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: Itraconazole

Cited by 105 publications

References 34 publications

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

PREPERATION AND CHARACTERIZATION OF Β-Cyclodextrin INCLUSION COMPLEXES ORAL TABLETS CONTAINING POORLY WATER SOLUBLE GLIMIPIRIDE USING FREEZE DRYING METHOD

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